Assay Detail
Binding
CHEMBL4424133
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Inhibition of TEL/AXL (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by SRB assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery of a potent tyrosine kinase AXL inhibitor bearing the 3-((2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yl)amino)pyrazine core.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.77 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4581972 | — | — | 1 | 8.52 |
| CHEMBL4576727 | — | — | 1 | 8.37 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 8.07 |
| CHEMBL4516515 | — | — | 1 | 8.02 |
| CHEMBL4529955 | — | — | 1 | 6.99 |
| CHEMBL4519811 | — | — | 1 | 6.67 |
| CHEMBL4462288 | — | — | 1 | - |
| CHEMBL4592943 | — | — | 1 | - |
| CHEMBL4475960 | — | — | 1 | - |
| CHEMBL4578043 | — | — | 1 | - |
| CHEMBL4524568 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4581972 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4576727 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL3301622 | GILTERITINIB | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL4516515 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL4529955 | — | IC50 | = | 102.5 | nM | 6.99 |
| CHEMBL4519811 | — | IC50 | = | 213.9 | nM | 6.67 |
| CHEMBL4462288 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4592943 | — | IC50 | > | 200.0 | nM | - |
| CHEMBL4475960 | — | IC50 | > | 200.0 | nM | - |
| CHEMBL4578043 | — | IC50 | > | 200.0 | nM | - |
| CHEMBL4524568 | — | IC50 | < | 0.3 | nM | - |